Plural Double Bonds Between Ring Members Of The Oxazole Ring Patents (Class 548/247)
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Publication number: 20110237595Abstract: The present invention is directed to compounds and compositions for the treatment of neurological diseases that cause neurogenic and neuropathic pain, inflammatory diseases, renal ischaemia, cardiovascular disease and other pathologies caused by the presence of endogenous cannabinoids and or other substrates resulting from the metabolic activities of fatty acid amido hydrolase (FAAH). These compounds are represented by the formula (I): wherein A, n, R1, R7 and R8 are as defined herein.Type: ApplicationFiled: June 9, 2011Publication date: September 29, 2011Applicant: SANOFI-AVENTISInventors: Ahmed ABOUABDELLAH, Regine BARTSCH-LI, Christian HOORNAERT, Antoine RAVET
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Patent number: 8026255Abstract: This invention is concerned with compounds of the formula and pharmaceutically acceptable salts thereof. The invention further relates to pharmaceutical compositions containing such compounds, to a process for their preparation and to their use for the treatment and/or prevention of diseases which are associated with the modulation of SST receptors subtype 5.Type: GrantFiled: May 10, 2010Date of Patent: September 27, 2011Assignee: Hoffman-La Roche Inc.Inventors: Alfred Binggeli, Andreas D. Christ, Hans P. Maerki, Rainer E. Martin
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Publication number: 20110223093Abstract: This invention relates to sulfur functionalized ionic liquid compounds that are useful in methods of carbon dioxide or sulfur dioxide removal to which they may be applied.Type: ApplicationFiled: March 11, 2011Publication date: September 15, 2011Applicant: E.I. DU PONT DE NEMOURS AND COMAPNYInventor: MARK A. SCIALDONE
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Publication number: 20110207937Abstract: The present invention relates to the discovery that specific human taste receptors in the T2R taste receptor family respond to particular bitter compounds present in, e.g., coffee. Also, the invention relates to the discovery of specific compounds and compositions containing that function as bitter taste blockers and the use thereof as bitter taste blockers or flavor modulators in, e.g., coffee and coffee flavored foods, beverages and medicaments. Also, the present invention relates to the discovery of a compound that antagonizes numerous different human T2Rs and the use thereof in assays and as a bitter taste blocker in compositions for ingestion by humans and animals.Type: ApplicationFiled: March 18, 2011Publication date: August 25, 2011Applicant: Senomyx, Inc.Inventors: Xiaodong LI, Andrew Patron, Catherine Tachdjian, Hong Xu, Qing Li, Alexey Pronin, Guy Servant, Lan Zhang, Thomas Brady, Vincent Darmohusodo, Melissa Arellano, Victor Selchau, Brett Weylan Ching, Donald S. Karanewsky, Paul Brust, Jing Ling, Wen Zhao, Chad Priest
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Publication number: 20110207788Abstract: The invention relates to 5-ring heteroaromatic compounds of general formula (I), their use for the treatment and/or prevention of diseases, and medicaments containing same.Type: ApplicationFiled: August 21, 2006Publication date: August 25, 2011Inventors: Wilhelm Amberg, Astrid Netz, Andreas Kling, Michael Ochse, Udo Lange, Andreas Haupt, Francisco Javier Garcia-Ladona, Wolfgang Wernet, Alfred Hahn
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Publication number: 20110207714Abstract: The biphenyic compounds of formula (I) are serotonin modulators useful in the treatment of serotonin-mediated diseases.Type: ApplicationFiled: October 29, 2009Publication date: August 25, 2011Inventors: Nicholas I. Carruthers, Brock T. Shireman, Vi T. Tran, Victoria D. Wong, Jill A. Jablonowski, Wenying Chai
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Patent number: 8003654Abstract: The invention relates to novel sulfonamide compounds of the formula (I) and their use as orexin receptor antagonists.Type: GrantFiled: April 10, 2007Date of Patent: August 23, 2011Assignee: Actelion Pharmaceuticals Ltd.Inventors: Hamed Aissaoui, Christoph Boss, Markus Gude, Ralf Koberstein, Thierry Sifferlen, Cornelia Zumbrunn Acklin
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Patent number: 8003648Abstract: The present invention provides compounds useful, for example, for treating metabolic disorders in a subject. Such compounds have the general formula I: where the definitions of the variables are provided herein. The present invention also provides compositions that include, and methods for using, the compounds in preparing medicaments and for treating metabolic disorders such as, for example, type II diabetes.Type: GrantFiled: November 5, 2009Date of Patent: August 23, 2011Assignee: Amgen Inc.Inventors: Hilary Beck, Paul Dransfield, Zice Fu, Jonathan B. Houze, XianYun Jiao, Todd J. Kohn, SuJen Lai, Jinqian Liu, Jiwen Liu, Zhihua Ma, Julio C. Medina, Michael J. Schmitt, Rajiv Sharma, Wang Shen, Marc Vimolratana, Yingcai Wang, Zhongyu Wang
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Publication number: 20110201555Abstract: The invention provides a compound of formula (I) or a pharmaceutically acceptable ester, amide, solvate or salt thereof, including a salt of such an ester or amide, and a solvate of such an ester, amide or salt. The invention also provides also provides the use of such compounds in the treatment or prophylaxis of a condition associated with a disease or disorder associated with estrogen receptor activity. wherein R1, R2, R3, R4, R5, R6, R7, R8, R9 , R10 and R11 are as defined in the specification.Type: ApplicationFiled: September 18, 2009Publication date: August 18, 2011Inventors: Patrik Rhönnstad, Theresa Apelqvist, Mattias Wennerstål, Aiping Cheng, Sandra Gordon
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Patent number: 7998994Abstract: Solid forms of (1R,2S,3R)-1-(2-(isoxazol-3-yl)-1H-imidazol-4-yl)butane-1,2,3,4-tetraol and hydrates thereof are disclosed, as well as compositions comprising them and methods of their use.Type: GrantFiled: June 16, 2009Date of Patent: August 16, 2011Assignee: Lexicon Pharmaceuticals, Inc.Inventors: Hugh Alfred Burgoon, Suzanne Marie Buttar, Christopher Stephen Frampton
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Publication number: 20110190247Abstract: In its many embodiments, the present invention provides a novel class of cyclopropylchromene derivatives as modulators of a2C adrenergic receptor, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more conditions associated with the a2C adrenergic receptors using such compounds or pharmaceutical compositions.Type: ApplicationFiled: August 3, 2009Publication date: August 4, 2011Applicant: Schering CorporationInventors: Younong Yu, Manuel De Lera Ruiz, Christopher W. Boyce, Kevin D. McCormick
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Publication number: 20110190294Abstract: The invention provides a compound of formula (I) or a pharmaceutically acceptable ester, amide, carbamate, solvate or salt thereof, including a salt of such an ester, amide or carbamate, and a solvate of such an ester, amide, carbamate or salt. The invention also provides also provides the use of such compounds in the treatment or prophylaxis of a condition associated with a disease or disorder associated with estrogen receptor activity, wherein R1, R2, R3, R4, R5 and R6 are as defined in the specification.Type: ApplicationFiled: April 16, 2009Publication date: August 4, 2011Inventors: Patrik Rhönnstad, Elisabet Kallin, Theresa Apelqvist, Mattias Wennerstål, Aiping Cheng
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Patent number: 7989450Abstract: Isoxazole derivatives, in particular diarylisoxazole derivatives inhibitors of cyclooxygenase (COX), in particular cyclooxygenase-1 (COX-1), their pharmaceutical compositions, the process for their preparation and their use for the chemoprevention and treatment of inflammatory syndromes and in the prevention and treatment of carcinomas, in particular intestinal, ovarian and cutaneous carcinomas, in the treatment of pain syndromes, in particular after surgery, and in the cardiovascular field as antithrombotics/vasoprotectives/cardioprotectives.Type: GrantFiled: January 11, 2008Date of Patent: August 2, 2011Assignees: Universita' Degli Studi Di Bari, Universita' Degli Studi “G.D.'Annunzio”—ChietiInventors: Antonio Scilimati, Paola Vitale, Leonardo Di Nunno, Paola Patrignani, Stefania Tacconelli, Marta Luciana Capone
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Patent number: 7989461Abstract: The present invention comprises a new class of compounds capable of modulating Raf kinase and, accordingly, useful for treatment of Raf kinase mediated diseases, including melanomas, tumors and other cancer-related conditions. The compounds have a general Formula I wherein R1 is and A1, A2, A3, A4, X, Z, Z?, R1, R2, R3, R4, R5 and R6 are defined herein. The invention further comprises pharmaceutical compositions, methods for treatment of Raf kinase mediated diseases, and intermediates and processes useful for the preparation of compounds of the invention.Type: GrantFiled: December 20, 2006Date of Patent: August 2, 2011Assignee: Amgen Inc.Inventors: Frenel F. De Morin, Jian J. Chen, Stephen Hitchcock, Gang Liu, Nick A. Paras, Jeffrey Petkus, Adrian L. Smith, Andrew Tasker, Jiawang Zhu
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Publication number: 20110183939Abstract: The present invention provides a novel P2X3 and/or P2X2/3 receptor antagonist. A compound represented by the formula (I); wherein Z1 is optionally protected hydroxy, etc.; Z2 is —C(?O)—, etc.; Z3a and Z3b are taken together ?O or ?S; t is an integer of 0 to 4; R4a and R4b are each independently, hydrogen or substituted or unsubstituted lower alkyl, etc.; m and n are each independently an integer of 0 to 2; k is an integer of 0 or 1; Ring A is an aromatic carbocyclic ring or a heterocyclic ring, etc.; B is aromatic carbocyclic ring-diyl or heterocyclic ring-diyl, etc.; R1a and R1b are each independently halogen, hydroxy, substituted or unsubstituted lower alkyl, etc.; R2 is substituted or unsubstituted alkyl, etc.; R3 is substituted or unsubstituted alkyl, substituted or unsubstituted aryl or a substituted or unsubstituted heterocyclic group, etc.; or its pharmaceutically acceptable salt, or a solvate thereof is provided.Type: ApplicationFiled: September 24, 2009Publication date: July 28, 2011Applicant: SHIONOGI & CO., LTD.Inventors: Hiroyuki Kai, Yoshiyuki Taoda, Takeshi Endoh, Tohru Horiguchi, Kentaro Asahi, Hiroyuki Tobinaga
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Publication number: 20110178042Abstract: The invention relates to a compound of formula (I): or a pharmaceutically acceptable salt thereof, thereof, wherein: G is a group of formula (II); and pharmaceutically acceptable salts, prodrugs, hydrates, or solvates, thereof, wherein A, B. L1-L4 A, B, R1-R4 and m are as defined herein. The invention also relates to pharmaceutical compositions comprising the compounds of formula (I) and their use in treating a bacterial infection.Type: ApplicationFiled: September 1, 2009Publication date: July 21, 2011Applicant: Pfizer Inc.Inventors: Matthew F. Brown, Charles F. Donovan, Edmund L. Eilsworth, Denton W. Hoyer, Timothy A. Johnson, Manjinder S. Lall, Chris Lim-Berakis, Sean T. Murphy, Debra A. Sherry, Clarke B. Taylor, Joseph S. Warmus
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Publication number: 20110178133Abstract: The present invention relates generally to novel calcimimetic compounds and pharmaceutical compositions comprising them. The invention also relates to methods of treating of diseases or disorders related to the function of the calcium sensing receptor using the compounds represented in Formula I.Type: ApplicationFiled: October 15, 2008Publication date: July 21, 2011Inventors: Thomas S. Coulter, Christopher H. Fotsch, Chiara Ghiron, Paul E. Harrington, Michael G. Kelly, Philip Miller, Gilbert M. Rishton, David J. St.Jean, JR., David J. Semin
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Publication number: 20110172279Abstract: The present invention is directed to N-hydroxyamidino compounds which are modulators of indoleamine 2,3-dioxygenase (IDO), as well as compositions and pharmaceutical methods thereof.Type: ApplicationFiled: March 23, 2011Publication date: July 14, 2011Inventors: Andrew P. Combs, Brian M. Glass, Richard B. Sparks, Eddy Wai Tsun Yue
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Patent number: 7977371Abstract: Objects of the present invention are to study on the synthesis of a novel pyrrole derivative having a ureido group and an aminocarbonyl group as substituents or a salt thereof, to find a pharmacological effect of the derivative or a salt thereof, and to find a medicinal agent which has a prophylactic and/or therapeutic effect on a retinal disease or the like through oral administration. A compound represented by the general formula (1) or a salt thereof has an inhibitory activity against the production of interleukin-6 and/or an inhibitory effect on choroidal neovascularization, and is therefore useful as a prophylactic and/or therapeutic agent for a disease associated with interleukin-6, an ocular inflammatory disease and/or a retinal disease.Type: GrantFiled: February 26, 2008Date of Patent: July 12, 2011Assignee: Santen Pharmaceutical Co., Ltd.Inventors: Kenji Kawashima, Hiroshi Enomoto, Noriko Ishizaka, Minoru Yamamoto, Kazuhiro Kudou, Masaaki Murai, Takaaki Inaba, Kazuyoshi Okamoto
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Patent number: 7968726Abstract: Methods of preparing compounds of formula I are disclosed:Type: GrantFiled: June 16, 2009Date of Patent: June 28, 2011Assignee: Lexicon Pharmaceuticals, Inc.Inventors: Jason Guohua Chen, Weifeng Hu, Renmao Liu, Yuelie Lu, Wenxue Wu, Xiaogen Yang
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Publication number: 20110152295Abstract: Heteroaromatic compounds of structural formula I are selective inhibitors of stearoyl-coenzyme A delta-9 desaturase (SCD1) relative to other known stearoyl-coenzyme A desaturases. The compounds of the present invention are useful for the prevention and treatment of conditions related to abnormal lipid synthesis and metabolism, including cardiovascular disease, such as atherosclerosis; obesity; diabetes; neurological disease; metabolic syndrome; insulin resistance; and liver steatosis.Type: ApplicationFiled: September 2, 2009Publication date: June 23, 2011Inventors: Jean-Philippe Leclerc, Chun Sing Li, Yeeman K. Ramtohul
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Patent number: 7956074Abstract: The present invention is concerned with isoxazol-4-yl-oxadiazole derivatives of formula wherein R1, R2, and R3, are as defined in the specification and pharmaceutically acceptable acid addition salts thereof. This class of compounds has high affinity and selectivity for GABA A ?5 receptor binding sites and might be useful as cognitive enhancer or for the treatment of cognitive disorders like Alzheimer's disease.Type: GrantFiled: April 13, 2009Date of Patent: June 7, 2011Assignee: Hoffman-La Roche Inc.Inventors: Bernd Buettelmann, Bo Han, Henner Knust, Andreas Koblet, Andrew Thomas
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Patent number: 7951827Abstract: Novel dicationic 3,5-diphenylisoxazole compounds are described. Synthetic routes to these novel compounds are provided. Several of the compounds displayed in vitro activity versus Trypanosoma brucei brucei and Plasmodium falciparum comparable to that of furamidine. A majority of the novel compounds also were less toxic to VERO cells than furamidine.Type: GrantFiled: May 2, 2006Date of Patent: May 31, 2011Assignee: The University of North Carolina at Chapel HillInventors: Richard R. Tidwell, Svetlana M. Bakunova, Stanislav Bakunov, Donald A. Patrick
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Patent number: 7947718Abstract: Certain isoxazole compounds are histamine H3 modulators useful in the treatment of histamine H3 receptor mediated diseases.Type: GrantFiled: September 15, 2009Date of Patent: May 24, 2011Assignee: Janssen Pharmaceutica NVInventors: Nicholas I. Carruthers, Chandravadan R. Shah, Devin M. Swanson
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Patent number: 7943778Abstract: This invention provides, but is not limited to, novel oleanolic acid derivatives having the formula: wherein the variables are defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds, methods and intermediates useful for making the compounds, and methods of using the compounds and compositions.Type: GrantFiled: April 20, 2009Date of Patent: May 17, 2011Assignee: Reata Pharmaceuticals, Inc.Inventors: Xin Jiang, Xiaofeng Liu, Jack Greiner, Stephen S. Szucs, Melean Visnick
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Publication number: 20110112142Abstract: The invention provides a pharmaceutical composition comprising a compound of formula (I) or a pharmaceutically acceptable ester, amide, solvate or salt thereof, including a salt of such an ester or amide, and a solvate of such an ester, amide or salt: wherein R3 is selected from the group consisting of ORA; —CHO; —C(O)C1-4alkyl; —C(O)phenyl; —O—C(O)RA; and N(RB)2; R6 is selected from certain cyclic groups defined in the specification; and the remaining groups are defined in the specification; together with a pharmaceutically acceptable carrier. Most of the compounds are novel. The invention also provides the use of such compounds in the treatment or prophylaxis of a condition associated with a disease or disorder associated with estrogen receptor activity.Type: ApplicationFiled: April 8, 2009Publication date: May 12, 2011Inventors: Daniel Nöteberg, Elisabet Kallin, Mattias Wennerstål
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Patent number: 7939671Abstract: The present invention relates to the discovery that specific human taste receptors in the T2R taste receptor family respond to particular bitter compounds present in, e.g., coffee. Also, the invention relates to the discovery of specific compounds and compositions containing that function as bitter taste blockers and the use thereof as bitter taste blockers or flavor modulators in, e.g., coffee and coffee flavored foods, beverages and medicaments. Also, the present invention relates to the discovery of a compound that antagonizes numerous different human T2Rs and the use thereof in assays and as a bitter taste blocker in compositions for ingestion by humans and animals.Type: GrantFiled: August 19, 2008Date of Patent: May 10, 2011Assignee: Senomyx, Inc.Inventors: Xiaodong Li, Andrew Patron, Catherine Tachdjian, Hong Xu, Qing Li, Alexey Pronin, Guy Servant, Lan Zhang, Thomas Brady, Vincent Darmohusodo, Melissa Arellano, Victor Selchau, Brett Weylan Ching, Donald S. Karanewsky, Paul Brust, Jing Ling, Wen Zhao, Chad Priest
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Patent number: 7939690Abstract: The present invention relates to novel compounds of formula [I], wherein R1 represents heteroaryl, at least one substituent among R5, R6 and R7 represent —SR12, —S(O)R12 or —S(O)2R12 and the remaining substituents are as defined in the claims, that act as chemical uncouplers. Compounds of the invention are useful inter alia, in the treatment, including prevention, of obesity, diabetes and a number of diseases associated therewith.Type: GrantFiled: November 15, 2007Date of Patent: May 10, 2011Assignee: High Point Pharmaceuticals, LLCInventors: Anders Klarskov Petersen, Preben Houlberg Olesen, Lise Brown Christiansen, Flemming Elmelund Nielsen
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Publication number: 20110105460Abstract: [Problem] A compound, which can be used for preventing or treating diseases, in which 11?-hydroxysteroid dehydrogenase type 1 (11?-HSD1) is concerned, in particular, diabetes, insulin resistance, dementia, schizophrenia and depression, is provided. [Means for Solution] It was found that a triazole derivative, in which one of the 3- and 5-positions of the triazole ring has (di)alkylmethyl or cycloalkyl, each of which is substituted with —O— (aryl or a heterocyclic group, each of which may be substituted, or lower alkylene-cycloalkyl), and the other thereof has aryl, a heterocyclic group or cycloalkyl, each of which may be substituted, or a pharmaceutically acceptable salt thereof exhibits potent 11?-HSD1 inhibitory action. From the above, the triazole derivative of the present invention can be used for preventing or treating diabetes, insulin resistance, dementia, schizophrenia and depression.Type: ApplicationFiled: July 2, 2009Publication date: May 5, 2011Applicant: ASTELLAS PHARMA INC.Inventors: Seiji Yoshimura, Noriyuki Kawano, Tomoaki Kawano, Daisuke Sasuga, Takanori Koike, Hideyuki Watanabe, Hiroki Fukudome, Nobuyuki Shiraishi, Ryosuke Munakata, Hiroaki Hoshii, Kayoko Mihara
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Patent number: 7935725Abstract: Aryl-substituted bridged or fused diamine compounds, pharmaceutical compositions containing them, and methods of using the compounds and the pharmaceutical compositions for leukotriene A4 hydrolase (LTA4H or LTA4H) modulation and for the treatment of disease states, disorders, and conditions mediated by LTA4H activity, such as allergy, asthma, autoimmune diseases, pruritis, inflammatory bowel disease, ulcerative colitis, and cardiovascular disease, including atherosclerosis and prevention of myocardial infarction.Type: GrantFiled: October 30, 2008Date of Patent: May 3, 2011Assignee: Janssen Pharmaceutica NVInventors: Scott D. Bembenek, Wendy Eccles, Laurent Gomez, Cheryl A. Grice, Aaron M. Kearney, Adrienne M. Landry-Bayle, Taraneh Mirzadegan, Alejandro Santillán, Jr.
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Publication number: 20110092496Abstract: A compound represented by the formula (I) (wherein R1, R2, R3 and R4 are as defined in the description), a tautomer, prodrug or pharmaceutically acceptable salt of the compound or a solvate thereof.Type: ApplicationFiled: November 29, 2010Publication date: April 21, 2011Applicant: Nissan Chemical Industries, Ltd.Inventors: Katsuaki MIYAJI, Kazufumi Yanagihara, Yukihiro Shigeta, Shunsuke Iwamoto, Masato Horikawa, Yutaka Hirokawa, Shingo Owada, Satoshi Nakano, Hirofumi Ota, Norihisa Ishiwata
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Publication number: 20110092512Abstract: The present invention relates to compounds of formula (I) as well as pharmaceutically acceptable salts thereof. The are useful as HSL inhibitors and may, for example, be used in treatment of diabetes, metabolic syndrome, dyslipidemia, atherosclerosis, and obesity.Type: ApplicationFiled: October 8, 2010Publication date: April 21, 2011Inventors: Jean Ackermann, Stephan Brugger, Aurelia Conte, Daniel Hunziker, Werner Neidhart, Matthias Nettekoven, Tanja Schulz-Gasch, Stanley Wertheimer
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Patent number: 7923470Abstract: The present invention is concerned with novel sulfonamides of formula I wherein R1, R2, Ar, Hetaryl, m and n are as described in the description and claims. The compounds are orexin receptor antagonists, useful in the treatment of disorders, in which orexin pathways are involved.Type: GrantFiled: July 21, 2009Date of Patent: April 12, 2011Assignee: Hoffmann-La Roche Inc.Inventors: Henner Knust, Matthias Nettekoven, Emmanuel Pinard, Olivier Roche, Mark Rogers-Evans
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Publication number: 20110082164Abstract: Described herein are compounds that are antagonists of lysophosphatidic receptor(s). Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such antagonists, alone and in combination with other compounds, for treating LPA-dependent or LPA-mediated conditions or diseases.Type: ApplicationFiled: September 29, 2010Publication date: April 7, 2011Applicant: AMIRA PHARMACEUTICALS, INC.Inventors: Ryan CLARK, Brian Andrew STEARNS, Lucy ZHAO, Thomas Jon SEIDERS, Deborah VOLKOTS, Jeannie M. ARRUDA
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Publication number: 20110082181Abstract: Described herein are compounds that are antagonists of lysophosphatidic receptor(s). Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such antagonists, alone and in combination with other compounds, for treating LPA-dependent or LPA-mediated conditions or diseases.Type: ApplicationFiled: October 1, 2010Publication date: April 7, 2011Applicant: Amira Phamaceuticals, Inc.Inventors: Thomas Jon SEIDERS, Lucy Zhao, Jeannie M. Arruda, Brian Andrew Stearns, Yen Pham Truong, Jill Melissa Scott, John Howard Hutchinson, Nicholas Simon Stock, Deborah Volkots
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Publication number: 20110077409Abstract: Cyano-substituted sulfilimines are produced efficiently and in high yield from the corresponding sulfides by reaction with cyanamide and hypochlorite.Type: ApplicationFiled: November 18, 2010Publication date: March 31, 2011Inventors: David E. Podhorez, Ronald Ross, JR., James R. McConnell
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Publication number: 20110071196Abstract: Compounds of formula (I) are disclosed. Compounds according to the invention bind to and are agonists, antagonists or inverse agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.Type: ApplicationFiled: September 15, 2010Publication date: March 24, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Alessandra BARTOLOZZI, Doris RIETHER, Renee M. ZINDELL, Patricia AMOUZEGH, Nigel James BLUMIRE, Monika ERMANN, Innocent MUSHI, Robert John SCOTT
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Patent number: 7906538Abstract: Novel trifluoromethanesulfonanilide oxime ether compounds useful for controlling endo and/or ectoparasites in the environment are provided, together with methods of making the same, and methods of using the inventive compounds to treat parasite infestations in vivo or ex vivo.Type: GrantFiled: October 31, 2007Date of Patent: March 15, 2011Assignee: Schering-Plough Animal Health CorporationInventors: Adam Gerhardt Meyer, Kevin Norman Winzenberg, David G. Sawutz, Andris Juris Liepa
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Patent number: 7906657Abstract: Novel 1,5-diphenylpyrazole derivatives of the formula (I) in which R1-R6 have the meanings indicated in claim 1, are HSP90 inhibitors and can be used for the preparation of a medicament for the treatment of diseases in which the inhibition, regulation and/or modulation of HSP90 plays a role.Type: GrantFiled: April 20, 2007Date of Patent: March 15, 2011Assignee: Merck Patent Gesellschaft MIT Beschraenkter HaftungInventors: Hans-Michael Eggenweiler, Michael Wolf, Hans-Peter Buchstaller, Christian Sirrenberg
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Publication number: 20110059938Abstract: The present invention encompasses compounds of general formula (1) wherein the groups R2 to R4, L, Q and n are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, and the use thereof for preparing a medicament having the above-mentioned properties.Type: ApplicationFiled: November 15, 2010Publication date: March 10, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Steffen STEURER, Peter ETTMAYER, Andreas MANTOULIDIS, Ioannis SAPOUNTZIS, Martin STEEGMAIER
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Publication number: 20110059893Abstract: The invention relates to compounds of structural formula (I): or a pharmaceutically acceptable salt, solvate, clathrate, and prodrug thereof, wherein Ra, Rb, and R2 are defined herein. These compounds inhibit tubulin polymerization and/or target vasculature and are useful for treating proliferative disorders, such as cancer.Type: ApplicationFiled: September 16, 2010Publication date: March 10, 2011Inventors: Lijun Sun, Christopher Borella, Hao Li, Jun Jiang, Shoujun Chen, Keizo Koya, Takayo Inoue, Zhenjian Du, Kevin Foley, Yaming Wu, Mei Zhang, Weiwen Ying
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Patent number: 7902201Abstract: The invention relates to isoxazolo-pyrazine derivatives and their pharmaceutically acceptable salts having affinity and selectivity for the GABA A ?5 receptor binding site, their manufacture, and pharmaceutical compositions containing them. The compounds of the present invention are inverse agonists of GABAA?5. The invention also relates to methods for enhancing cognition and for treating cognitive disorders like Alzheimer's disease.Type: GrantFiled: May 27, 2010Date of Patent: March 8, 2011Assignee: Hoffmann-La Roche Inc.Inventors: Bernd Buettelmann, Roland Jakob-Roetne, Henner Knust, Andrew Thomas
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Publication number: 20110053980Abstract: The present invention relates to indane-amine compounds of general formula (I) and compositions thereof, methods for their preparation, and the use of said compounds for the preparation of a medicament for the treatment of humans or animals.Type: ApplicationFiled: July 4, 2008Publication date: March 3, 2011Applicant: LABORATORIOS DEL DR. ESTEVE, S.A.Inventors: Monica Garcia-Lopez, Antonio Torrens-Jover
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Publication number: 20110046378Abstract: Disclosed here in are compounds and methods of diagnosing Alzheimer's Disease or a predisposition thereto in a mammal, the method comprising administering to the mammal a diagnostically effective amount of a radiolabeled compound, wherein the compound is selected from the group consisting of radiolabeled flavones, coumarins, carbazoles, quinolinones, chromenones, imidazoles and triazoles derivatives, allowing the compound to distribute into the brain tissue, and imaging the brain tissue, wherein an increase in binding of the compound to the brain tissue compared to a normal control level of binding indicates that the mammal is suffering from or is at risk of developing Alzheimer's DiseaseType: ApplicationFiled: February 17, 2009Publication date: February 24, 2011Applicant: SIEMENS MEDICAL SOLUTIONS USA, INC.Inventors: Hartmuth C. Kolb, Joseph C. Walsh, Qianwa Liang, Brian A. Duclos, Wei Zhang, Peter J.H. Scott, Kai Chen, Zhiyong Gao, Tieming Zhao, Vani P. Mocharla, Dhanalakshmi Kasi, Gang Chen, Eric Wang, Anjana Sinha, Chunfang Xia, Henry Clifton Padgett, Farhad Karimi
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Publication number: 20110046147Abstract: The invention relates to 17beta-hydroxysteroid dehydrogenase type 1 (17betaHSD1) inhibitors, the preparation thereof and the use thereof for the treatment and prophylaxis of hormone-related, especially estrogen-related or androgen-related, diseases.Type: ApplicationFiled: August 22, 2008Publication date: February 24, 2011Applicant: UNIVERSITAT DES SAARLANDESInventors: Rolf Hartmann, Martin Frotscher, Sandrine Oberwinkler, Emmanuel Bey
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Publication number: 20110046129Abstract: 2-Phenylethylamino substituted carboxamide derivatives and their use as sodium and/or calcium channel modulators useful in preventing, alleviating and curing a wide range of pathologies are presented.Type: ApplicationFiled: September 9, 2010Publication date: February 24, 2011Applicant: Newron Pharmaceuticals S.p.A.Inventors: Florian Thaler, Mauro Napoletano, Cibele Sabido-David, Ermanno Moriggi, Carla Caccia, Laura Faravelli, Alessandra Restivo, Patricia Salvati
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Patent number: 7893066Abstract: The present invention discloses pyrido[2,3-B]pyrazinones having the structure of Formula I for use as inhibitors of stearoyl-CoA desaturase. The compounds are useful in treating and/or preventing various human diseases, mediated by stearoyl-CoA desaturase (SCD) enzymes, especially diseases related to abnormal lipid levels, cardiovascular disease, diabetes, obesity, oily skin conditions, metabolic syndrome, and the like.Type: GrantFiled: April 9, 2008Date of Patent: February 22, 2011Assignee: Gilead Palo Alto, Inc.Inventors: Dmitry Koltun, Jeff Zablocki, Eric Parkhill, Andrei Glushkov, Natalya Vasilevich, Timur Zilbershtein, Alexey Ivanov, Jeffrey Chisholm
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Patent number: 7888509Abstract: One aspect of the invention relates to 1,8-diarylnaphthalene compounds. In certain embodiments, a compound of the invention is an N-oxide of a 1,8-diarylnaphthalene. In certain embodiments, the aryl group is an optionally substituted acridyl group. In certain embodiments, a compound of the invention is a single steroisomer. In certain embodiments, a compound of the invention is a single enantiomer. Another aspect of the present invention relates to a method of detecting the presence of an analyte in a sample by monitoring the fluorescence of a compound of the invention in a sample. In certain embodiments, the analyte is a metal ion. Another aspect of the present invention relates to a method of determining the enantiomeric purity of an analyte by monitoring the fluorescence of a compound of the invention in the presence of the analyte. In certain embodiments, the analyte is a compound that is capable of hydrogen bonding.Type: GrantFiled: November 1, 2004Date of Patent: February 15, 2011Assignee: Georgetown UniversityInventors: Christian Wolf, Xuefeng Mei
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Publication number: 20110034483Abstract: The present invention is directed to 2-aminoimidazole compounds of formula (I) which are inhibitors of the beta-secretase enzyme and that are useful in the treatment of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which the beta-secretase enzyme is involved.Type: ApplicationFiled: February 18, 2009Publication date: February 10, 2011Inventors: Ivory D. Hills, Craig A. Coburn, Samuel L. Graham, Keith P. Moore, Philippe G. Nantermet, Hemaka A. Rajapakse, Shawn J. Stachel, Hong Zhu
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Publication number: 20110028485Abstract: Novel 1,5-diphenylpyrazole derivatives of the formula (I) in which R1-R6 have the meanings indicated in claim 1, are HSP90 inhibitors and can be used for the preparation of a medicament for the treatment of diseases in which the inhibition, regulation and/or modulation of HSP90 plays a role.Type: ApplicationFiled: September 16, 2010Publication date: February 3, 2011Inventors: Hans-Michael EGGENWEILER, Michael Wolf, Hans-Peter Buchstaller, Christian Sirrenberg